CO5150235A1 - ROACETIC ANTIOBESITY TIROMIMETRIC AGENTS CONTAINING THEM - Google Patents
ROACETIC ANTIOBESITY TIROMIMETRIC AGENTS CONTAINING THEMInfo
- Publication number
- CO5150235A1 CO5150235A1 CO00014834A CO00014834A CO5150235A1 CO 5150235 A1 CO5150235 A1 CO 5150235A1 CO 00014834 A CO00014834 A CO 00014834A CO 00014834 A CO00014834 A CO 00014834A CO 5150235 A1 CO5150235 A1 CO 5150235A1
- Authority
- CO
- Colombia
- Prior art keywords
- lower alkyl
- hydrogen
- cycloalkyl
- hydroxy
- trifluoromethyl
- Prior art date
Links
- 230000003579 anti-obesity Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 208000008589 Obesity Diseases 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000001721 carbon Chemical group 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 235000020824 obesity Nutrition 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Valve Device For Special Equipments (AREA)
- Discharging, Photosensitive Material Shape In Electrophotography (AREA)
- Refinement Of Pig-Iron, Manufacture Of Cast Iron, And Steel Manufacture Other Than In Revolving Furnaces (AREA)
- Saccharide Compounds (AREA)
- Medicinal Preparation (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
Abstract
La invención se refiere a composiciones farmacéuticas y a métodos útiles en el tratamiento de la obesidad, cuyos métodos comprenden administrar a un animal, incluyendo el hombre o un animal de compañía, necesitado de tal tratamiento, una cantidad eficaz de un compuesto de la fórmula estructural:<EMI FILE="00014834_1" ID="1" IMF=JPEG >o una sal farmacéuticamente aceptable, racemato o enantiómero del mismo, en la que R es hidroxi, hidroxi esterificado o hidroxi eterificado; R1 y R2 son, independientemente, halógeno, trifluorometilo o alquilo inferior; R3 es halógeno, trifluorometilo, alquilo inferior, arilo, aril-alquilo inferior, cicloalquilo o cicloalquil-alquilo inferior, arilmetilo carbocíclico, aroilo carbocíclico, arilhidroximetilo carbocíclico; o R3 es el radical <EMI FILE="00014834_2" ID="2" IMF=JPEG >en el que R8 es hidrógeno, alquilo inferior, arilo, cicloalquilo, arilalquilo inferior o cicloalquil- alquilo inferior; R9 es hidróxi o aciloxi; R10 es hidrógeno o alquilo inferior; o R9 y R10 tomados junto con el átomo de carbono al que están unidos forman un grupo carbonilo; R4 es hidrógeno, halógeno, trifluorometilo o alquilo inferior; R5 y R6 son, independienmente, hidrógeno o alquilo inferior o R5 y R6, tomados junto con el átomo de carbono al que están unidos forman un grupo carbonilo; X es O, S o -NR7; R7 es hidrógeno o alquilo inferior; W es 0 o S, y Z es carboxilo o carboxilo derivatizado como un éster o una amida farmacéuticamente aceptable.La invención proporciona, además, composiciones farmacéuticas y métodos de utilización de los compuestos de fórmula estructural (I), o las sales farmacéuticamente aceptable, racematos y enantiómeros de los mismos, en combinación con un agente anorético, para el tratamiento de la obesidad.The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity, whose methods comprise administering to an animal, including man or a companion animal, in need of such treatment, an effective amount of a compound of the structural formula: <EMI FILE = "00014834_1" ID = "1" MFI = JPEG> or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are independently halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical <EMI FILE = "00014834_2" ID = "2" IMF = JPEG> in which R8 is hydrogen, lower alkyl, aryl, cycloalkyl, lower arylalkyl or cycloalkyl-lower alkyl; R9 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10 taken together with the carbon atom to which they are attached form a carbonyl group; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; R5 and R6 are independently hydrogen or lower alkyl or R5 and R6, taken together with the carbon atom to which they are attached form a carbonyl group; X is O, S or -NR7; R7 is hydrogen or lower alkyl; W is 0 or S, and Z is carboxyl or carboxyl derivatized as a pharmaceutically acceptable ester or amide. The invention further provides pharmaceutical compositions and methods of using the compounds of structural formula (I), or pharmaceutically acceptable salts, racemates and enantiomers thereof, in combination with an abnormal agent, for the treatment of obesity.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12201599P | 1999-03-01 | 1999-03-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5150235A1 true CO5150235A1 (en) | 2002-04-29 |
Family
ID=22400061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00014834A CO5150235A1 (en) | 1999-03-01 | 2000-03-01 | ROACETIC ANTIOBESITY TIROMIMETRIC AGENTS CONTAINING THEM |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US6344481B1 (en) |
| EP (1) | EP1036564B1 (en) |
| JP (1) | JP2000256190A (en) |
| KR (1) | KR100368354B1 (en) |
| AT (1) | ATE282410T1 (en) |
| AU (1) | AU1635300A (en) |
| CA (1) | CA2299972C (en) |
| CO (1) | CO5150235A1 (en) |
| DE (1) | DE60015831T2 (en) |
| ES (1) | ES2233282T3 (en) |
| HU (1) | HUP0000921A3 (en) |
| IL (1) | IL134382A0 (en) |
| NZ (1) | NZ503122A (en) |
| PE (1) | PE20001539A1 (en) |
| ZA (1) | ZA200001000B (en) |
Families Citing this family (69)
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| US20050261362A1 (en) * | 2004-03-22 | 2005-11-24 | The Regents Of The University Of California | Method of increasing endogenous adiponectin and leptin production |
| WO2003077847A2 (en) * | 2002-03-12 | 2003-09-25 | Merck & Co., Inc. | Substituted amides |
| US6825209B2 (en) | 2002-04-15 | 2004-11-30 | Research Triangle Institute | Compounds having unique CB1 receptor binding selectivity and methods for their production and use |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| CA2502511A1 (en) * | 2002-10-18 | 2004-05-29 | Pfizer Products Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040122033A1 (en) * | 2002-12-10 | 2004-06-24 | Nargund Ravi P. | Combination therapy for the treatment of obesity |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
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| US20080255084A1 (en) | 2005-10-21 | 2008-10-16 | Randy Lee Webb | Combination of Organic Compounds |
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| JP5319518B2 (en) | 2007-04-02 | 2013-10-16 | Ｍｓｄ株式会社 | Indoledione derivative |
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| US9401828B2 (en) | 2010-05-20 | 2016-07-26 | Kandou Labs, S.A. | Methods and systems for low-power and pin-efficient communications with superposition signaling codes |
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| AU2014235209B2 (en) | 2013-03-15 | 2018-06-14 | Bausch Health Ireland Limited | Guanylate cyclase receptor agonists combined with other drugs |
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| CN105764916B (en) | 2013-06-05 | 2021-05-18 | 博士医疗爱尔兰有限公司 | Ultrapure agonists of guanylate cyclase C, methods of making and using the same |
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| KR20190104524A (en) | 2016-11-21 | 2019-09-10 | 바이킹 테라퓨틱스 인코포레이티드 | Treatment method of sugar accumulation disease |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| WO2018118670A1 (en) | 2016-12-20 | 2018-06-28 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
| EA201992703A1 (en) | 2017-06-05 | 2020-04-15 | Вайкинг Терапьютикс, Инк. | COMPOSITIONS FOR TREATING FIBROSIS |
| US12090252B2 (en) | 2017-09-14 | 2024-09-17 | Riken | Method for producing retinal tissues |
| KR20200138283A (en) | 2018-03-22 | 2020-12-09 | 바이킹 테라퓨틱스 인코포레이티드 | Crystalline forms, and methods of preparing compounds in crystalline form |
| MX2021005904A (en) | 2018-11-20 | 2021-09-08 | Tes Pharma S R L | INHIBITORS OF a-AMINO-ß-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE. |
| US12102646B2 (en) | 2018-12-05 | 2024-10-01 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis and inflammation |
| US20220170098A1 (en) | 2019-03-13 | 2022-06-02 | Sumitomo Dainippon Pharma Co., Ltd. | Method for Evaluating Quality of Transplant Neural Retina, and Transplant Neural Retina Sheet |
| CA3194226A1 (en) | 2020-09-11 | 2022-03-17 | Riken | Complex containing neural retina-containing cell aggregates and matrix, and method for manufacturing same |
| EP4201428A4 (en) | 2020-09-11 | 2024-09-11 | Sumitomo Pharma Co., Ltd. | MEDIUM FOR TISSUE TRANSPLANTATION |
| JPWO2023090427A1 (en) | 2021-11-19 | 2023-05-25 | ||
| CN118772088B (en) * | 2024-06-14 | 2025-10-03 | 北京农学院 | 2-Butenoic acid lactone thioacetate compounds and preparation method and application thereof |
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-
2000
- 2000-01-20 US US09/488,110 patent/US6344481B1/en not_active Expired - Fee Related
- 2000-02-03 IL IL13438200A patent/IL134382A0/en unknown
- 2000-02-03 AT AT00300830T patent/ATE282410T1/en not_active IP Right Cessation
- 2000-02-03 DE DE60015831T patent/DE60015831T2/en not_active Expired - Fee Related
- 2000-02-03 ES ES00300830T patent/ES2233282T3/en not_active Expired - Lifetime
- 2000-02-03 EP EP00300830A patent/EP1036564B1/en not_active Expired - Lifetime
- 2000-02-11 AU AU16353/00A patent/AU1635300A/en not_active Abandoned
- 2000-02-25 JP JP2000049507A patent/JP2000256190A/en active Pending
- 2000-02-28 HU HU0000921A patent/HUP0000921A3/en unknown
- 2000-02-28 PE PE2000000162A patent/PE20001539A1/en not_active Application Discontinuation
- 2000-02-28 KR KR10-2000-0009860A patent/KR100368354B1/en not_active Expired - Fee Related
- 2000-02-29 NZ NZ503122A patent/NZ503122A/en unknown
- 2000-02-29 CA CA002299972A patent/CA2299972C/en not_active Expired - Fee Related
- 2000-02-29 ZA ZA200001000A patent/ZA200001000B/en unknown
- 2000-03-01 CO CO00014834A patent/CO5150235A1/en unknown
-
2001
- 2001-10-16 US US09/978,980 patent/US6555578B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DE60015831T2 (en) | 2005-12-15 |
| US6344481B1 (en) | 2002-02-05 |
| PE20001539A1 (en) | 2001-01-08 |
| CA2299972C (en) | 2003-08-19 |
| EP1036564B1 (en) | 2004-11-17 |
| JP2000256190A (en) | 2000-09-19 |
| DE60015831D1 (en) | 2004-12-23 |
| CA2299972A1 (en) | 2000-09-01 |
| HU0000921D0 (en) | 2000-04-28 |
| NZ503122A (en) | 2001-11-30 |
| IL134382A0 (en) | 2001-04-30 |
| ZA200001000B (en) | 2001-08-29 |
| EP1036564A1 (en) | 2000-09-20 |
| ATE282410T1 (en) | 2004-12-15 |
| HUP0000921A3 (en) | 2004-06-28 |
| US20020035153A1 (en) | 2002-03-21 |
| KR100368354B1 (en) | 2003-01-24 |
| AU1635300A (en) | 2000-09-07 |
| ES2233282T3 (en) | 2005-06-16 |
| KR20010006712A (en) | 2001-01-26 |
| HUP0000921A2 (en) | 2000-12-28 |
| US6555578B2 (en) | 2003-04-29 |
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